Tag: M.W=200-250

Wang, Huai-Wei; Qiao, Yu-Han; Wu, Jia-Xue; Wang, Qiu-Ping; Tian, Meng-Xin; Li, Yong-Fei; Yao, Qing-Xia; Li, Da-Cheng; Dou, Jian-Min; Lu, Yi published the artcile< RhIII-Catalyzed C-H (Het)arylation/Vinylation of N-2,6-Difluoroaryl Acrylamides>, Product Details of C11H16BNO2, the main research area is arylboronate difluorophenyl acrylamide rhodium catalyst regioselective diastereoselective arylation; aryl difluorophenyl acrylamide preparation; vinylboronate difluorophenyl acrylamide rhodium catalyst regioselective diastereoselective vinylation; vinyl difluorophenyl acrylamide preparation.

RhIII-catalyzed sp2 C-H cross-coupling of acrylamides with organoboron reactants was accomplished using a com.available N-2,6-difluoroaryl acrylamide auxiliary. A broad range of aryl and vinyl boronates as well as a variety of heterocyclic boronates with strong coordinating ability served as the coupling partners. This transformation proceeded under moderate reaction conditions with excellent functional group tolerance and high regioselectivity.

Organic Letters published new progress about Acrylamides Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Product Details of C11H16BNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Guo-Xi; Chen, Yuwen; Zhu, Jie-Ji; Song, Jia-Yu; Tang, Shan-Shun; Ma, Dongge; Tong, Qing-Xiao published the artcile< Rational design of pyridine-containing emissive materials for high performance deep-blue organic light-emitting diodes with CIEy ∼ 0.06>, Reference of 329214-79-1, the main research area is rational design pyridine containing emissive material high performance deep.

Charge balance does matter for emission materials to obtain high-performance organic light-emitting diodes (OLEDs), and it is well-known that the electron-transporting ability is inferior to the hole-transporting for the majority of organic emitting materials, especially for blue-emitting compounds Hence, systematically investigating the effect of the electron-withdrawing group on fluorophore is of vital importance. In this study, we designed and synthesized two deep-blue phenanthro[9,10-d]imidazole (PI) based materials named DPy-PPI and DmPy-PPI by using pyridine-containing groups as electron acceptor as well as adjusting the conjugation length. The photophys., theor., thermal and electrochem. properties of the compounds were investigated systematically, and the relationship between the conjugation length of substituent groups on phenanthroimidazole and the EL performance was clarified. Both of them exhibited good thermal stability and high photoluminescence quantum yields. Non-doped devices based on DPy-PPI and DmPy-PPI as emitter achieved deep-blue emissions with the Commission Internationale de L’Eclairage (CIE) index of (0.14, 0.06) and (0.15, 0.08) and high external quantum efficiencies (EQEmax) of 4.24% and 3.74%, resp. Meanwhile, using DPy-PPI and DmPy-PPI as the host materials, yellow-orange phosphorescent organic light-emitting diodes (PHOLEDs) were fabricated with EQEmax, CEmax and PEmax of 20.55%, 63.86 cd/A, 37.08 lm/W and 18.14%, 55.84 cd/A, 32.47 lm/W, resp. Furthermore, the red PHOLEDs were also constructed using DPy-PPI and DmPy-PPI as the host with EQEmax, CEmax and PEmax of 14.53%, 17.04 cd/A, 18.51 lm/W and 16.62%, 23.58 cd/A, 21.16 lm/W, resp. And we believe this work can provide some insight suggestions for scientific researchers to design deep-blue emitting materials.

Dyes and Pigments published new progress about Blue-emitting electroluminescent devices. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Reference of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dyck, Brian; Grigoriadis, Dimitri E.; Gross, Raymond S.; Guo, Zhiqiang; Marinkovic, Dragan; McCarthy, James R.; Moorjani, Manisha; Regan, Collin F.; Saunders, John; Schwaebe, Michael K.; Szabo, Tomas; Williams, John P.; Zhang, Xiaohu; Bozigian, Haig; Chen, Ta Kung published the artcile< Potent, Orally Active Corticotropin-Releasing Factor Receptor-1 Antagonists Containing a Tricyclic Pyrrolopyridine or Pyrazolopyridine Core>, Application of C9H9Cl2NO2, the main research area is oral CRF1 receptor antagonist tricyclic pyrrolopyridine pyrazolopyridine core preparation.

Two new classes of tricyclic-based corticotropin-releasing factor (CRF1) receptor-1 antagonists were designed by constraining known 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine ligands. Pyrrole- and pyrazole-based mols. 19g and 22a, resp., were discovered that potently bind the recombinant CRF1 receptor (Ki = 3.5, 2.9 nM) and inhibit adrenocorticotropic hormone (ACTH) release from rat pituitary cell culture (IC50 = 14, 6.8 nM). These compounds show good oral bioavailability (F = 24%, 7.0%) and serum half-lives in rats (t1/2 = 6.3, 12 h) and penetrate the rat brain ([brain]/[plasma] = 0.27, 0.52) but tend toward large volumes of distribution (VD = 38, 44 L kg-1) and rapid clearances (CL = 70, 43 mL min-1 kg-1). When given orally, both the pyrazole and the pyrrole leads dose-dependently inhibit stress-induced ACTH release in vivo. ACTH reductions of 84-86% were observed for 30 mg kg-1 doses.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier (penetration). 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Application of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Di Fabio, Romano; Arban, Roberto; Bernasconi, Giovanni; Braggio, Simone; Blaney, Frank E.; Capelli, Anna M.; Castiglioni, Emiliano; Donati, Daniele; Fazzolari, Elettra; Ratti, Emiliangelo; Feriani, Aldo; Contini, Stefania; Gentile, Gabriella; Ghirlanda, Damiano; Sabbatini, Fabio M.; Andreotti, Daniele; Spada, Simone; Marchioro, Carla; Worby, Angela; St-Denis, Yves published the artcile< Dihydropyrrole[2,3-d]pyridine Derivatives as Novel Corticotropin-Releasing Factor-1 Antagonists: Mapping of the Receptor Binding Pocket by in Silico Docking Studies>, COA of Formula: C9H9Cl2NO2, the main research area is pyrrolo pyridine preparation CRF1 antagonist antidepressant SAR.

In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochem. properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent Ph ring and the nature of the heterocyclic moieties present in the upper region of the mol. Selective and potent compounds have been discovered endowed with reduced ClogP with respect to compounds known in the literature. Of particular relevance was the finding that the in vitro affinity of the series was maintained by reducing the overall lipophilicity. The results achieved by this exploration enabled the formulation of a novel hypothesis on the nature of the receptor binding pocket of this class of CRF-1 receptor antagonists, making use of in silico docking studies of the putative nonpeptidic antagonist binding site set up in house by homol. modeling techniques.

Journal of Medicinal Chemistry published new progress about Antidepressants. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, COA of Formula: C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Shengdong; Huang, Haiyun; Roisnel, Thierry; Bruneau, Christian; Fischmeister, Cedric published the artcile< Base-Free Dehydrogenation of Aqueous and Neat Formic Acid with Iridium(III) Cp*(dipyridylamine) Catalysts>, Safety of 2-Bromo-N,N-dimethylpyridin-4-amine, the main research area is preparation crystal structure iridium cyclopentadiynyl dipyridylamine complex; cyclic voltammetry iridium cyclopentadiynyl dipyridylamine complex; Dehydrogenation formic acid iridium cyclopentadiynyl dipyridylamine complex catalyst; N ligands; dehydrogenation; energy conversion; hydrogen; iridium.

The selective dehydrogenation of formic acid by iridium(III) Cp*(dipyridylamine) catalysts is reported. The electron-enriched catalyst [IrIIICp*{(4-dimethylaminopyridin-2-yl-κN)(pyridin-2′-yl-κN)amine}(OSO3)] gave the best performances enabling the base free dehydrogenation of aqueous and neat formic acid. In both cases the reaction was selective with no carbon monoxide detectable. The IrIII complex demonstrated latent behavior, which may be of practical utility. Exptl. results suggest an outer-sphere interaction with the ligand.

ChemSusChem published new progress about Crystal structure. 396092-82-3 belongs to class pyridine-derivatives, and the molecular formula is C7H9BrN2, Safety of 2-Bromo-N,N-dimethylpyridin-4-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhou, Sen; Hou, Xiaoya; Yang, Kai; Guo, Minjie; Zhao, Wentao; Tang, Xiangyang; Wang, Guangwei published the artcile< Direct Synthesis of N-Difluoromethyl-2-pyridones from Pyridines>, Name: 1,2-Di(pyridin-2-yl)disulfane, the main research area is difluoromethylpyridone difluoromethylquinolinone preparation.

A novel method for the synthesis of N-difluoromethyl-2-pyridones was described. This protocol enables the synthesis of N-difluoromethyl-2-pyridones from readily available pyridines using mild reaction conditions that are compatible with a wide range of functional groups. The preliminary mechanistic study revealed that N-difluoromethylpyridinium salts were the key intermediates to complete this conversion.

Journal of Organic Chemistry published new progress about One-pot synthesis. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Name: 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xiao, Xuan; Wang, Kewei; Zong, Qingyu; Tu, Yalan; Dong, Yansong; Yuan, Youyong published the artcile< Polyprodrug with glutathione depletion and cascade drug activation for multi-drug resistance reversal>, HPLC of Formula: 2127-03-9, the main research area is polydisulfide prodrug glutathione depletion multidrug resistance reversal; Glutathione response; Multidrug resistance; poly(disulfide).

High intracellular glutathione (GSH) levels play an important role in multidrug resistance (MDR) in cancer cells. It remains challenging to develop a drug delivery system that is simultaneously capable of GSH depletion and drug activation for multidrug resistance reversal. Herein, we designed a polyprodrug (denoted as PSSD) based on poly(disulfide) conjugated with doxorubicin (DOX) on the polymer side chains that exhibits GSH depletion and cascade DOX activation for drug resistance reversal. The poly(disulfide) backbone with a high disulfide d. depletes intracellular antioxidant GSH via the disulfide-thiol exchange reaction to disrupt intracellular redox homeostasis in cells. Simultaneously, DOX can be activated through a cascade reaction, and degradation of the poly(disulfide) backbone further facilitates its drug release. Therefore, poly(disulfide) can be used as a GSH scavenger to reverse MDR as well as a prodrug backbone to target high intracellular GSH levels in cancer cells, providing a general strategy for drug resistance reversal.

Biomaterials published new progress about Antitumor agent resistance. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Longjia; Liu, Zibo; Tang, Shanyu; Li, Jiao; Ren, Xuanhe; Yang, Guanyu; Li, Heng; Yuan, Bingxin published the artcile< Amphiphilic ligands for Cu-catalyzed aerobic oxidation to synthesize 9-fluorenones in water>, Product Details of C10H6Cl2N2, the main research area is fluorenone preparation; fluorene aerobic oxidation copper catalyst.

A series of amphiphilic PEG-functionalized nitrogen ligands were developed for the highly efficient copper-catalyzed aerobic oxidation of 9-fluorenes, with mol. oxygen as the sole oxidant in neat water to afford 9-fluorenones I [R = H, 2-NH2, 2-I, etc.]. A broad range of functional groups were well tolerated and thus offered the opportunity for further functionalization.

Catalysis Communications published new progress about Fluorenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1762-41-0 belongs to class pyridine-derivatives, and the molecular formula is C10H6Cl2N2, Product Details of C10H6Cl2N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shirazi, Seyed Mohammad Hossein; Mokhtari, Javad; Mirjafary, Zohreh published the artcile< A new method for the synthesis of abiraterone drug catalyzed by Pd-NPs@Zn-MOF as efficient reusable catalyst>, Related Products of 329214-79-1, the main research area is abiraterone palladium nanoparticle heterogeneous catalyst Suzuki Miyaura.

The present work provides a novel process for the preparation of abiraterone drug in a Suzuki-Miyaura coupling approach by a new heterogeneous palladium catalyst, Pd-NPs@Zn-MOF, which has been synthesized by one-step encapsulation in nanoporous metal-organic framework Zn-MOF under a temperature control program for the first time. Pd-NPs@Zn-MOF were characterized by transmission electron microscopy (TEM), X-Ray powder diffraction (XRD), BET surface area anal., inductively coupled plasma (ICP)-optical emission spectrometry (OES), and XPS.

Applied Organometallic Chemistry published new progress about Emission spectroscopy. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Related Products of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Darwish, Shaban; Sadeghiani, Neda; Fong, Shirley; Mozaffari, Saghar; Hamidi, Parinaz; Withana, Thimanthi; Yang, Sun; Tiwari, Rakesh Kumar; Parang, Keykavous published the artcile< Synthesis and antiproliferative activities of doxorubicin thiol conjugates and doxorubicin-SS-cyclic peptide>, Safety of 1,2-Di(pyridin-2-yl)disulfane, the main research area is human embryonic kidney ovarian fibrosarcoma leukemia; cyclopeptide preparation antitumor doxorubicin fluorescence cellular uptake chemotherapy antiproliferative; Anticancer; Cardiotoxicity; Cellular uptake; Cyclic peptide; Disulfide; Doxorubicin; Thiol.

Myocardial toxicity and drug resistance caused by drug efflux are major limitations of doxorubicin (Dox)-based chemotherapy. Dox structure modification could be used to develop conjugates with an improved biol. profile, such as antiproliferative activity and higher cellular retention. Thus, Dox thiol conjugates, Dox thiol (Dox-SH), thiol-reactive Dox-SS-pyridine (SS = disulfide), and a Dox-SS-cell-penetrating cyclic peptide, Dox-SS-[C(WR)4K], were synthesized. Dox was reacted with Traut’s reagent to generate Dox-SH. Cytotoxicity of the compounds was examined in human embryonic kidney (HEK-293), human ovarian cancer (SKOV-3), human fibrosarcoma (HT-1080), and human leukemia (CCRF-CEM) cells. These data indicate that Dox-SH, Dox-SS-Pyr, and Dox-SS-[C(WR)4K] have the potential to be further examined as Dox alternatives and anticancer agents.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Safety of 1,2-Di(pyridin-2-yl)disulfane.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem